EP0037011B1 - Ointment bases for dermatological and cosmetic use - Google Patents
Ointment bases for dermatological and cosmetic use Download PDFInfo
- Publication number
- EP0037011B1 EP0037011B1 EP81102009A EP81102009A EP0037011B1 EP 0037011 B1 EP0037011 B1 EP 0037011B1 EP 81102009 A EP81102009 A EP 81102009A EP 81102009 A EP81102009 A EP 81102009A EP 0037011 B1 EP0037011 B1 EP 0037011B1
- Authority
- EP
- European Patent Office
- Prior art keywords
- skin
- vaseline
- weight
- ointment base
- percent
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired
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- 239000003883 ointment base Substances 0.000 title claims abstract description 22
- 239000002537 cosmetic Substances 0.000 title claims description 9
- 239000002904 solvent Substances 0.000 claims abstract description 23
- 229940099259 vaseline Drugs 0.000 claims abstract description 22
- 239000003921 oil Substances 0.000 claims abstract description 13
- 238000002844 melting Methods 0.000 claims abstract description 10
- HMMGMWAXVFQUOA-UHFFFAOYSA-N octamethylcyclotetrasiloxane Chemical compound C[Si]1(C)O[Si](C)(C)O[Si](C)(C)O[Si](C)(C)O1 HMMGMWAXVFQUOA-UHFFFAOYSA-N 0.000 claims abstract description 8
- XMSXQFUHVRWGNA-UHFFFAOYSA-N Decamethylcyclopentasiloxane Chemical compound C[Si]1(C)O[Si](C)(C)O[Si](C)(C)O[Si](C)(C)O[Si](C)(C)O1 XMSXQFUHVRWGNA-UHFFFAOYSA-N 0.000 claims abstract description 7
- KPUWHANPEXNPJT-UHFFFAOYSA-N disiloxane Chemical class [SiH3]O[SiH3] KPUWHANPEXNPJT-UHFFFAOYSA-N 0.000 claims abstract description 7
- UQEAIHBTYFGYIE-UHFFFAOYSA-N hexamethyldisiloxane Chemical compound C[Si](C)(C)O[Si](C)(C)C UQEAIHBTYFGYIE-UHFFFAOYSA-N 0.000 claims abstract description 7
- 239000004200 microcrystalline wax Substances 0.000 claims abstract description 6
- 235000019808 microcrystalline wax Nutrition 0.000 claims abstract description 6
- 230000008018 melting Effects 0.000 claims abstract description 5
- 150000001298 alcohols Chemical class 0.000 claims abstract description 3
- 239000000470 constituent Substances 0.000 claims description 3
- 125000004432 carbon atom Chemical group C* 0.000 claims description 2
- 239000000654 additive Substances 0.000 abstract description 8
- 235000019271 petrolatum Nutrition 0.000 abstract description 8
- 238000005406 washing Methods 0.000 abstract description 7
- 239000004264 Petrolatum Substances 0.000 abstract description 5
- 229940066842 petrolatum Drugs 0.000 abstract description 5
- 230000000996 additive effect Effects 0.000 abstract description 2
- 238000001704 evaporation Methods 0.000 abstract description 2
- 230000008020 evaporation Effects 0.000 abstract description 2
- VQLYBLABXAHUDN-UHFFFAOYSA-N bis(4-fluorophenyl)-methyl-(1,2,4-triazol-1-ylmethyl)silane;methyl n-(1h-benzimidazol-2-yl)carbamate Chemical compound C1=CC=C2NC(NC(=O)OC)=NC2=C1.C=1C=C(F)C=CC=1[Si](C=1C=CC(F)=CC=1)(C)CN1C=NC=N1 VQLYBLABXAHUDN-UHFFFAOYSA-N 0.000 abstract 1
- 231100000344 non-irritating Toxicity 0.000 abstract 1
- 210000003491 skin Anatomy 0.000 description 53
- 238000002360 preparation method Methods 0.000 description 26
- 239000000203 mixture Substances 0.000 description 11
- 239000007788 liquid Substances 0.000 description 8
- -1 siloxanes Chemical class 0.000 description 7
- 239000007787 solid Substances 0.000 description 7
- 239000000243 solution Substances 0.000 description 5
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 5
- 238000007792 addition Methods 0.000 description 4
- 230000000694 effects Effects 0.000 description 4
- 239000000126 substance Substances 0.000 description 4
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 description 3
- 239000004909 Moisturizer Substances 0.000 description 3
- 206010040880 Skin irritation Diseases 0.000 description 3
- 238000001816 cooling Methods 0.000 description 3
- 238000009826 distribution Methods 0.000 description 3
- 229930195733 hydrocarbon Natural products 0.000 description 3
- 150000002430 hydrocarbons Chemical class 0.000 description 3
- 230000005923 long-lasting effect Effects 0.000 description 3
- 230000001333 moisturizer Effects 0.000 description 3
- 230000036556 skin irritation Effects 0.000 description 3
- 231100000475 skin irritation Toxicity 0.000 description 3
- 230000000475 sunscreen effect Effects 0.000 description 3
- 239000000516 sunscreening agent Substances 0.000 description 3
- DSEKYWAQQVUQTP-XEWMWGOFSA-N (2r,4r,4as,6as,6as,6br,8ar,12ar,14as,14bs)-2-hydroxy-4,4a,6a,6b,8a,11,11,14a-octamethyl-2,4,5,6,6a,7,8,9,10,12,12a,13,14,14b-tetradecahydro-1h-picen-3-one Chemical compound C([C@H]1[C@]2(C)CC[C@@]34C)C(C)(C)CC[C@]1(C)CC[C@]2(C)[C@H]4CC[C@@]1(C)[C@H]3C[C@@H](O)C(=O)[C@@H]1C DSEKYWAQQVUQTP-XEWMWGOFSA-N 0.000 description 2
- 239000004215 Carbon black (E152) Substances 0.000 description 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
- 230000001464 adherent effect Effects 0.000 description 2
- 230000001166 anti-perspirative effect Effects 0.000 description 2
- 239000003213 antiperspirant Substances 0.000 description 2
- 238000003287 bathing Methods 0.000 description 2
- 230000000254 damaging effect Effects 0.000 description 2
- 239000003599 detergent Substances 0.000 description 2
- 238000004821 distillation Methods 0.000 description 2
- 239000000839 emulsion Substances 0.000 description 2
- 150000002191 fatty alcohols Chemical class 0.000 description 2
- 239000003205 fragrance Substances 0.000 description 2
- 230000007794 irritation Effects 0.000 description 2
- 239000010410 layer Substances 0.000 description 2
- 230000035515 penetration Effects 0.000 description 2
- 230000000144 pharmacologic effect Effects 0.000 description 2
- 229920001296 polysiloxane Polymers 0.000 description 2
- 230000005855 radiation Effects 0.000 description 2
- 210000002374 sebum Anatomy 0.000 description 2
- 239000000344 soap Substances 0.000 description 2
- CWERGRDVMFNCDR-UHFFFAOYSA-N thioglycolic acid Chemical compound OC(=O)CS CWERGRDVMFNCDR-UHFFFAOYSA-N 0.000 description 2
- 239000003440 toxic substance Substances 0.000 description 2
- 230000036572 transepidermal water loss Effects 0.000 description 2
- HIQIXEFWDLTDED-UHFFFAOYSA-N 4-hydroxy-1-piperidin-4-ylpyrrolidin-2-one Chemical compound O=C1CC(O)CN1C1CCNCC1 HIQIXEFWDLTDED-UHFFFAOYSA-N 0.000 description 1
- 206010000349 Acanthosis Diseases 0.000 description 1
- 206010020751 Hypersensitivity Diseases 0.000 description 1
- 239000004166 Lanolin Substances 0.000 description 1
- 239000006096 absorbing agent Substances 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 239000013543 active substance Substances 0.000 description 1
- 230000000172 allergic effect Effects 0.000 description 1
- 230000007815 allergy Effects 0.000 description 1
- CEGOLXSVJUTHNZ-UHFFFAOYSA-K aluminium tristearate Chemical compound [Al+3].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CEGOLXSVJUTHNZ-UHFFFAOYSA-K 0.000 description 1
- 229940063655 aluminum stearate Drugs 0.000 description 1
- 239000007864 aqueous solution Substances 0.000 description 1
- 208000010668 atopic eczema Diseases 0.000 description 1
- 230000005540 biological transmission Effects 0.000 description 1
- 238000009835 boiling Methods 0.000 description 1
- 230000000711 cancerogenic effect Effects 0.000 description 1
- 231100000315 carcinogenic Toxicity 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 150000008280 chlorinated hydrocarbons Chemical class 0.000 description 1
- 239000000084 colloidal system Substances 0.000 description 1
- 210000004087 cornea Anatomy 0.000 description 1
- 238000012937 correction Methods 0.000 description 1
- 239000006071 cream Substances 0.000 description 1
- 239000010779 crude oil Substances 0.000 description 1
- 230000007423 decrease Effects 0.000 description 1
- 235000014113 dietary fatty acids Nutrition 0.000 description 1
- 125000000118 dimethyl group Chemical group [H]C([H])([H])* 0.000 description 1
- 238000001035 drying Methods 0.000 description 1
- 239000003995 emulsifying agent Substances 0.000 description 1
- 210000002615 epidermis Anatomy 0.000 description 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 1
- 238000000605 extraction Methods 0.000 description 1
- 239000000194 fatty acid Substances 0.000 description 1
- 229930195729 fatty acid Natural products 0.000 description 1
- 150000004665 fatty acids Chemical class 0.000 description 1
- 230000002349 favourable effect Effects 0.000 description 1
- 235000013305 food Nutrition 0.000 description 1
- 210000004907 gland Anatomy 0.000 description 1
- 239000012456 homogeneous solution Substances 0.000 description 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
- 229940039717 lanolin Drugs 0.000 description 1
- 235000019388 lanolin Nutrition 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 238000002803 maceration Methods 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical class CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- 230000009965 odorless effect Effects 0.000 description 1
- 239000002674 ointment Substances 0.000 description 1
- 210000000056 organ Anatomy 0.000 description 1
- 239000012188 paraffin wax Substances 0.000 description 1
- 235000019809 paraffin wax Nutrition 0.000 description 1
- 239000012437 perfumed product Substances 0.000 description 1
- 231100000760 phototoxic Toxicity 0.000 description 1
- 229920000036 polyvinylpyrrolidone Chemical class 0.000 description 1
- 239000001267 polyvinylpyrrolidone Chemical class 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 239000011252 protective cream Substances 0.000 description 1
- 230000001681 protective effect Effects 0.000 description 1
- 239000011241 protective layer Substances 0.000 description 1
- 150000004040 pyrrolidinones Chemical class 0.000 description 1
- 238000010992 reflux Methods 0.000 description 1
- 239000004576 sand Substances 0.000 description 1
- 210000001732 sebaceous gland Anatomy 0.000 description 1
- 230000037380 skin damage Effects 0.000 description 1
- 230000036620 skin dryness Effects 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 230000036561 sun exposure Effects 0.000 description 1
- 230000037072 sun protection Effects 0.000 description 1
- 239000002562 thickening agent Substances 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- 238000009834 vaporization Methods 0.000 description 1
- 230000008016 vaporization Effects 0.000 description 1
- 229920002554 vinyl polymer Polymers 0.000 description 1
- 239000000080 wetting agent Substances 0.000 description 1
- XOOUIPVCVHRTMJ-UHFFFAOYSA-L zinc stearate Chemical compound [Zn+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O XOOUIPVCVHRTMJ-UHFFFAOYSA-L 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/24—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/31—Hydrocarbons
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/58—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing atoms other than carbon, hydrogen, halogen, oxygen, nitrogen, sulfur or phosphorus
- A61K8/585—Organosilicon compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q17/00—Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
Definitions
- the invention relates to ointment bases for dermatological and cosmetic purposes based on Vaseline @ with the addition of siloxane.
- the ointment bases are intended for cosmetic or medicinal use on healthy, injured or diseased skin.
- the skin the largest organ in the human body, primarily serves to protect it from the environment.
- the integument is essentially exposed to three damaging effects: UV radiation, chemicals and an environment that is too dry or too humid.
- the skin must be protected against this. This can be done against UV radiation by avoiding sun exposure as far as possible and / or using sunscreen products, against too dry or too humid surroundings and partly. it also protects itself against chemicals through the sebum produced by the sebum glands and, to a much lesser extent, through the fat formed when the cells are horny.
- the activity of the sebaceous glands is hormonally controlled and decreases with age. For this reason, the supply of fat to the skin in older people is insufficient, which results in the importance of an increased supply of fat from outside.
- the skin fat is now largely removed by hygienic measures such as washing, bathing or showering, especially in the most washed areas of the skin such as hands and face.
- hygienic measures such as washing, bathing or showering, especially in the most washed areas of the skin such as hands and face.
- Unprotected skin suffers from a great loss of moisture due to the humidity caused by the cold - it dries out and painful skin cracks can occur.
- long-term exposure to water especially if its surface tension is greatly reduced by soaps or syndets, causes skin damage due to maceration (e.g. washer hands).
- Vaseline @ (regardless of whether white, yellow or red) is by far the best moisturizer (moisturizer)
- this effect is not based on a reduction in transepidermal water loss through occlusion, but on a pharmacological effect of Vaselin @ on the skin.Vaseli ® nfett is cosmetically extremely unsatisfactory, however, because it is poor in toughness the skin penetrates and adheres insufficiently to it so that it can be removed mechanically and easily by washing, and because of its consistency it is difficult to apply thinly, so that an unpleasant greasy and sticky layer is formed which is extremely annoying when working It is known that in addition to a certain skin-irritating effect, petroleum jelly @ also widens the epidermis (acanthosis) b can work.
- Vaseline @ This is an indication of the pharmacological effects of Vaseline @.
- the properties mentioned are evidently mainly due to the portions of the Vaseline @ boiling below 180 ° C at 2 mbar (see, for example, Schaaf, "Problems of basic dermatological research” 1969, p. 105 ff.).
- the low irritation residual fraction is difficult to distribute on the skin due to its toughness and is therefore cosmetically unsatisfactory.
- vaselins @ corresponding to the requirements of the pharmacopoeias do not have any toxic, carcinogenic or other damaging properties
- all vaselins @ commercially can be at least latently irritating to the skin, ie they can be unmixed Skin compatibility, but as soon as the colloidal system is changed by adding liquid substances in which petroleum jelly @ is soluble, low-molecular components, e.g.
- BE-B-1 134 478 also describes a skin protection ointment which consists of 45 to 60% by weight of a dimethyl and / or diphenylpolysiloxane with a viscosity of 150 to 350 centistokes, 15 to 30% by weight of zinc stearate and 25% by weight.
- % paraffinic ointment base is built up.
- the thereby siloxanes used are not volatile and remain on the skin while the siloxanes employed in this invention are volatile, that is, a smooth application of the agent to the skin is promoted, and after evaporation of the volatile siloxane solvent remains on the skin, a firmly adhering Vaseli ® nfilm in fine Distribution.
- the usual petrolatum NF as the ointment base are reproduced as petrolatum USP.
- only special VaseliB fractions the content of white oils of which is less than 20% by weight, are used.
- an antiperspirant stick which is composed of waxy fatty alcohol, astringent, volatile silicone and certain polyethoxylated fatty alcohols.
- an antiperspirant stick has to meet different requirements than an ointment base in which no astringent is provided, and moreover, in such a stick neither Vaseline @ according to the special invention is used with a content of white oils below 20% by weight.
- the object of the invention is to provide a physiologically harmless ointment base which is readily distributable and firmly adhering to the skin, which is free from irritation and offers long-lasting protection even with frequent washing.
- the ratio of Vaseline @ to solvent is preferably 30 to 70% by weight to 70 to 30% by weight.
- the weight ratio of solid to liquid at 20 to 25 ° C proportions is over 3, in particular 5 to 7.
- high-melting microcrystalline waxes are contained in the ointment base according to the invention.
- the present ointment base expediently has physiologically compatible lower alcohol as an additional component.
- the ointment bases according to the invention consist of physiologically harmless , whose white oil content is below 20% by weight.
- the white oils comprise the low-boiling, low-viscosity, skin-irritating components of Vaseline @. After the white oils have been separated off, for example by distillation, irritant-free Vaseli fractions are obtained.
- the Vaseli fractions preferably contain no portions with less than 20 carbon atoms in the molecule. Any Vaseline @ can be used to produce the Vaseline fractions used according to the invention.
- VaseliR fractions described above which have only a low content of white oils or from which the white oils have been separated to the stated content by distillation and thus have a low probability of possible skin irritation, leads to the use of the physiologically harmless ones which can be used according to the invention Solvents for stable, opaque, dermatologically inexpensive and cosmetically appealing preparations.
- Vaseli g fractions to be used which have a weight ratio of solid to 20 to 25 ° C liquid shares above. 3
- the ratio of solid to liquid at 20 to 25 ° C proportions should not exceed 10: 1.
- Such are preferably obtained by extraction of the crude distillate with halogenated, especially chlorinated hydrocarbons.
- the ointment bases according to the invention contain as solvents for the specified Hexamethyldisiloxane, octamethylcyclotetrasiloxane and / or decamethylcyclopentasiloxane.
- solvents for the specified Hexamethyldisiloxane, octamethylcyclotetrasiloxane and / or decamethylcyclopentasiloxane.
- These solvents are physiologically compatible and form with the in the heat, ie at or above the melting range of the Vaseli fraction, clear solutions.
- the solvents are preferably only limited in the soluble, so that like mixtures are formed.
- the solvents mentioned are volatile and do not remain on the skin. Volatility means that the solvents evaporate from the skin within a short time due to their low heat of vaporization.
- the solvents can be used both individually and in a mixture.
- the siloxanes used only serve as solvents in order to achieve a good distribution of the Vaseline @ on the skin, but do not remain on the skin due to the volatility and leave a protective layer after they evaporate on the skin. In addition to their inertness, the volatility of the solvents used is extremely important for the effectiveness of the preparations and the skin protection that can be achieved with them.
- Vaseline @ the liquid components of which are greatly reduced compared to the solid ones This will make it even better Preserve skin protection, as these preparations provide permanent skin protection even when exposed to detergents.
- a greasy gloss remaining on the skin when these preparations are used can be practically eliminated by increasing the proportion of high-melting constituents of the Vaseline @ by adding high-melting microcrystalline waxes without impairing the good spreadability of the preparation.
- High-melting microcrystalline waxes with a melting range of 85 to 95 ° C deliver excellent results.
- high-melting microcrystalline guards (melting point approx. 90 ° C) in the amount of 5 to 15% by weight, based on the sum of vasefine fraction and solvent white, opaque masses are obtained which adhere well to the skin and hardly any shine leave. This is surprising, since microcrystalline waxes are otherwise used to increase the gloss, particularly in the case of paraffin waxes.
- the preparations according to the invention can also contain further physiologically tolerable additives. Additions in small amounts, e.g. up to 5%, suitable. It is preferred to add physiologically acceptable lower alcohols, e.g. Ethyl and isopropyl alcohol. If small amounts of such additives are added in the production, then particularly easily spreadable, cosmetically appealing preparations are obtained which dry matt and not glossy and also have a cooling effect which is often desired. Furthermore, other customary additives can be contained in the preparations according to the invention, provided that they are physiologically unsuitable and are compatible with the solvents used. Examples of such additives are UV adsorbers, odorants and thickeners such as e.g.
- Ceresin, ozokerite, aluminum stearate, polyvinyl stearate and polyvinyl pyrrolidone derivatives then, to modify the feeling on the skin, isopropyl esters of fatty acids such as isopropyl myristate and lanolin derivatives.
- the total amount of additives present in the ointment base according to the invention should preferably not exceed 20% by weight, based on the sum of the vasetin fraction and the siloxane solvent.
- the preparations according to the invention have an excellent protective action for the skin.
- the preparations according to the invention are also particularly suitable as a commercial protective cream.
- the two components are warmed until a clear solution is obtained, after which the mixture is stirred cold.
- the components are heated until a clear solution is obtained, then the mixture is stirred until cold.
- the components are heated until a clear solution is obtained, then the mixture is stirred until cold.
- the first 3 parts are melted in a heatable vessel provided with a reflux condenser at approx. 95 ° C., and after a homogeneous solution has been formed, the octamethylcyclotetrasiloxane is added and the mixture is cooled with gentle stirring. After standing for 24 hours, a pure white lipogel is formed, which is easy to spread on the skin and very strongly hydrophobicizes the hands treated with it.
- the amount to be used is small: 0.3 to 0.5 g is generally sufficient for skin protection during a whole working day.
- the preparation is carried out in the same way as in Example 4.
- the preparation produced gives a particularly pleasant feeling on the skin.
- the preparation is carried out in the same manner as in Example 4.
- the preparation obtained can easily be spread on the skin to form a thin, matt-drying film, which remains on the skin as protection even after frequent washing.
- the components are heated until a clear solution is obtained, then the mixture is stirred until cold.
- the preparation obtained is easy to spread on the skin and provides long-lasting skin protection.
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- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Dermatology (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oil, Petroleum & Natural Gas (AREA)
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- Molecular Biology (AREA)
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Abstract
Description
Die Erfindung betrifft Salbengrundlagen für dermatologische und kosmetische Zwecke auf der Basis von Vaseline@ unter Zusatz von Siloxan. Die Salbengrundlagen sind zur kosmetischen oder medikamentösen Anwendung auf der gesunden, verletzten oder kranken Haut bestimmt.The invention relates to ointment bases for dermatological and cosmetic purposes based on Vaseline @ with the addition of siloxane. The ointment bases are intended for cosmetic or medicinal use on healthy, injured or diseased skin.
Die Haut, das größte Organ des menschlichen Körpers, dient primär dessen Schutz gegen die Umgebung. Das Integument ist im wesentlichen drei schädigenden Einwirkungen ausgesetzt: UV-Strahlung, Chemikalien und zu trockene oder zu feuchte Umgebung. Dagegen ist die Haut zu schützen. Gegen UV-Strahlung läßt sich dies tun, indem man Sonnenexposition möglichst vermeidet und/oder Sonnenschutzpräparate anwendet, gegen zu trockene oder zu feuchte Umgebung und z.T. auch gegen Chemikalien schützt sie sich durch das von den Talgdrüsen gebildete Sebum und zu einem allerdings viel geringeren Teil durch das bei der Verhornung der Zellen gebildete Fett. Die Tätigkeit der Talgdrüsen ist hormonell gesteuert und nimmt mit dem Alter ab. Deshalb ist die Fettversorgung der Haut beim älteren Menschen ungenügend, woraus sich die Wichtigkeit einer vermehrten Fettzufuhr von außen ergibt. Das Hautfett wird nun durch hygienische Maßnahmen wie Waschen, Baden oder Duschen weitgehend entfernt und dies insbesondere bei den am meisten gewaschenen Hautpartien wie Hände und Gesicht. Bei geringer, z.B. durch Kälte bedingter, Luftfeuchtigkeit erleidet die ungeschützte Haut einen starken Feuchtigkeitsverlust-sie trocknet aus, und es können schmerzhafte Hautrisse entstehen. Andererseits entstehen bei langandauernder Einwirkung von Wasser, insbesondere wenn dessen Oberflächenspannung durch Seifen oder Syndets stark herabgesetzt ist, Hautschäden durch Mazeration (z.B. Waschfrauenhände).The skin, the largest organ in the human body, primarily serves to protect it from the environment. The integument is essentially exposed to three damaging effects: UV radiation, chemicals and an environment that is too dry or too humid. The skin must be protected against this. This can be done against UV radiation by avoiding sun exposure as far as possible and / or using sunscreen products, against too dry or too humid surroundings and partly. it also protects itself against chemicals through the sebum produced by the sebum glands and, to a much lesser extent, through the fat formed when the cells are horny. The activity of the sebaceous glands is hormonally controlled and decreases with age. For this reason, the supply of fat to the skin in older people is insufficient, which results in the importance of an increased supply of fat from outside. The skin fat is now largely removed by hygienic measures such as washing, bathing or showering, especially in the most washed areas of the skin such as hands and face. At low, e.g. Unprotected skin suffers from a great loss of moisture due to the humidity caused by the cold - it dries out and painful skin cracks can occur. On the other hand, long-term exposure to water, especially if its surface tension is greatly reduced by soaps or syndets, causes skin damage due to maceration (e.g. washer hands).
Die kosmetische Industrie sucht Austrocknungszustände der Haut durch sogenannte Feuchtigkeitschremes (Moisturizer) zu beheben. Alle Cremes liegen als ÖI-in-Wasser- oder als Wasser-in-ÖI- bzw. Misch-Emulsionen vor. Sie enthalten Emulgatoren, welche das Durchdringen von Wasser und das Entfernen durch Waschen des aufgetrockneten Fettfilmes erleichtern. Diese Zubereitungen vermögen den transepidermalen Wasserverlust der Haut nur ungenügend zu unterbinden, und die erreichte Feuchthaltung der Haut ist unbefriedigend. Vaseline@ hingegen vermag den Wasserverlust der Haut weitgehend zu unterbinden. Vaseline@ ist ein eingetragenes Warenzeichen für aus Rohölen hergestelltes Petrolatum, das als Gelbe und Weiße Vaseline@ im Handel ist (vergl. "Römpps Chemie-Lexikon", 1977, Seite 3780). Kligman (siehe z.B. "Cosmetics and Toiletries", 93 (4) 27 (1978) hat denn auch wiederholt darauf hingewiesen, daß dieses Kohlenwasserstoffgemisch der Vaseline@ (ungeachtet, ob weiß, gelb oder rot) mit Abstand das beste Feuchthaltemittel (Moisturizer) sei; gleichzeitig ist er aber der Ansicht, daß diese Wirkung nicht auf einer Verminderung des transepidermalen Wasserverlustes durch Okklusion, sondern auf einer pharmakologischen Wirkung der Vaselin@ auf die Haut beruhe. Vaseli®nfett ist jedoch kosmetisch höchst unbefriedigend, weil es zufolge seiner Zähigkeit schlecht in die Haut eindringt und ungenügend auf ihr haftet, so daß es mechanisch und durch Waschen leicht wieder entfernbar ist. Weiterhin läßt es sich wegen seiner Konsistenz nur schwierig dünn auftragen, so daß sich eine unangenehme fettige und klebrige Schicht bildet, die beim Arbeiten äußerst störend ist. Es ist bekannt, daß die Vaseline@ neben einer gewissen hautreizenden Wirkung auch eine Epidermisverbreiterung (Akanthose) bewirken kann. Dies ist ein Hinweis auf die pharmakologische Wirkung der Vaseline@. Die erwähnten Eigenschaften kommen offenbar vorwiegend den unterhalb von 180°C bei 2 mbar siedenden Anteilen der Vaseline@ zu (siehe z.B. Schaaf, "Problems der dermatologischen Grundlagenforschung" 1969, S. 105 ff.). Die reizarme Restfraktion läßt sich wegen ihrer Zähigkeit nur schlecht auf der Haut verteilen und ist somit kosmetisch unbefriedigend.The cosmetic industry seeks to correct skin dryness by means of so-called moisturizers. All creams are available as oil-in-water or water-in-oil or mixed emulsions. They contain emulsifiers, which facilitate the penetration of water and the removal by washing the dried fat film. These preparations are insufficient to prevent transepidermal water loss from the skin, and the skin's moisturization is unsatisfactory. Vaseline @, on the other hand, can largely prevent water loss from the skin. Vaseline @ is a registered trademark for petrolatum made from crude oils, which is commercially available as yellow and white Vaseline @ (cf. "Römpps Chemie-Lexikon", 1977, page 3780). Kligman (see for example "Cosmetics and Toiletries", 93 (4) 27 (1978) has repeatedly pointed out that this hydrocarbon mixture of Vaseline @ (regardless of whether white, yellow or red) is by far the best moisturizer (moisturizer) At the same time, however, he is of the opinion that this effect is not based on a reduction in transepidermal water loss through occlusion, but on a pharmacological effect of Vaselin @ on the skin.Vaseli ® nfett is cosmetically extremely unsatisfactory, however, because it is poor in toughness the skin penetrates and adheres insufficiently to it so that it can be removed mechanically and easily by washing, and because of its consistency it is difficult to apply thinly, so that an unpleasant greasy and sticky layer is formed which is extremely annoying when working It is known that in addition to a certain skin-irritating effect, petroleum jelly @ also widens the epidermis (acanthosis) b can work. This is an indication of the pharmacological effects of Vaseline @. The properties mentioned are evidently mainly due to the portions of the Vaseline @ boiling below 180 ° C at 2 mbar (see, for example, Schaaf, "Problems of basic dermatological research" 1969, p. 105 ff.). The low irritation residual fraction is difficult to distribute on the skin due to its toughness and is therefore cosmetically unsatisfactory.
Aus "Lexikon der Hilfsstoffe für Pharmazie, Kosmetik und angrenzende Gebiete", (1971), Seite 615 bis 617, ist die Verwendung von Vaseline@, deren Hydrophobie nur von den Siliconen übertroffen wird, in Salbengrundlagen bekannt. Die Probleme der Hautreizung werden eingehend angesprochen. Obgleich angegeben wird, daß bestimmte, den Anforderungen der Arzneibücher entsprechende Vaselinen@ keine toxischen, carcinogegen oder sonstwie schädigende Eigenschaften besitzen, ist bekannt, daß alle Vaselinen@ des Handels, auch wenn sie Arzneibuchanforderungen entsprechen, zumindest latent hautreizend sein können, d.h. sie können unvermischt Hautverträglichkeit aufweisen, sobald aber das kolloidale System durch Zugabe flüssiger Stoffe, in denen Vaselinen@ löslich sind, verändert wird, können niedrigmolekulare Anteile, z.B. C1O―C18-Kohlenwasserstoffe, welche hautreizend sind, (vgl. "Cosmetics and Toiletries", 94, (8) 41, (1979) sich im ausblutenden Zusatzstoff anreichern und zur bekannten stechenden Hautreizung Anlaß geben. Demgegenüber haben sich die erfindungsgemäß eingesetzten Vaseiinfraktionen, aus denen die leicht flüchtigen Weißöle bis auf einen Gehalt von unter 20 Gew.% abgetrennt wurden, auch wenn sie in den speziellen Siloxanen gelöst sind und damit leichter in die Haut eindringen, als vollkommen reizfrei erwiesen. In "Römpps Chemie-Lexikon", 7. Auflage, (1976), S. 3223 ff. und "Kosmetik und Aerosole" in Seifen-Öle-Fette-Wachse, 100. Jg. Nr. 7/1974, S. 173 bis 177, werden ausschließlich lineare, praktisch nicht-flüchtige Dimethylsiloxane beschrieben, die bei Anwendung in Salbengrundlagen als wesentliche Bestandteile in dem auf der Haut verbleibenden Wirkstoffgemisch vorliegen, während die erfindungsgemäß eingesetzten speziellen Siloxane flüchtig sind und bei ihrer Anwendung nicht auf der Haut verbleiben, wobei nur der festhaftende Vaselillfilm in feiner Verteilung auf der Haut als Schutz vorliegt. Auch wird in der BE-B-1 134 478 eine Hautschutzalbe beschrieben, die aus 45 bis 60 Gew.% eines Dimethyl- und/oder Diphenylpolysiloxans mit einer Viskosität von 150 bis 350 Centistokes, 15 bis 30 Gew.% Zinkstearat und 25 Gew.% paraffinischer Salbengrundlage aufgebaut ist. Die dabei eingesetzten Siloxane sind nichtflüchtig und verbleiben auf der Haut, während die erfindungsgemäß eingesetzten Siloxane flüchtig sind, d.h. ein geschmeidiger Auftrag des Mittels auf die Haut wird begünstigt, und nach Abdampfen des flüchtigen Siloxan-Lösungsmittels verbleibt auf der Haut ein festhaftender Vaseli®nfilm in feiner Verteilung. In Remington's Pharmaceutical Science 15. Ausgabe, Mack Publishing Co., Eaton, Pa. USA, (1975), S. 1247-48, sind als Salbengrundlagen übliches Petrolatum NF als Petrolatum USP wiedergegeben. Gemäß der Erfindung werden jedoch nur spezielle VaseliBfraktionen, deren Gehalt an Weißölen unter 20 Gew.% liegt, eingesetzt.From "Lexicon of auxiliaries for pharmacy, cosmetics and related areas", (1971), pages 615 to 617, the use of Vaseline @, the hydrophobicity of which is only surpassed by the silicones, is known in ointment bases. The problems of skin irritation are addressed in detail. Although it is stated that certain vaselins @ corresponding to the requirements of the pharmacopoeias do not have any toxic, carcinogenic or other damaging properties, it is known that all vaselins @ commercially, even if they meet pharmacopoeia requirements, can be at least latently irritating to the skin, ie they can be unmixed Skin compatibility, but as soon as the colloidal system is changed by adding liquid substances in which petroleum jelly @ is soluble, low-molecular components, e.g. C 1O ―C 18 hydrocarbons, which are irritating to the skin (see "Cosmetics and Toiletries", 94 , (8) 41, (1979) accumulate in the bleeding-out additive and give rise to the known pungent skin irritation, while the vasein fractions used according to the invention, from which the volatile white oils have been separated down to a content of less than 20% by weight, also have when they are dissolved in the special siloxanes and thus easier to penetrate into the skin wrestle, proven to be completely irritation-free. In "Römpps Chemie-Lexikon", 7th edition, (1976), p. 3223 ff. And "Kosmetik und Aerosole" in Seifen-Öle-Fette-Wwachs, 100. vol. No. 7/1974, p. 173 bis 177, only linear, practically non-volatile dimethylsiloxanes are described which, when used in ointment bases, are present as essential constituents in the active substance mixture remaining on the skin, while the special siloxanes used according to the invention are volatile and do not remain on the skin when used, only the adherent Vaseli l oil film is present as a protection in fine distribution on the skin. BE-B-1 134 478 also describes a skin protection ointment which consists of 45 to 60% by weight of a dimethyl and / or diphenylpolysiloxane with a viscosity of 150 to 350 centistokes, 15 to 30% by weight of zinc stearate and 25% by weight. % paraffinic ointment base is built up. The thereby siloxanes used are not volatile and remain on the skin while the siloxanes employed in this invention are volatile, that is, a smooth application of the agent to the skin is promoted, and after evaporation of the volatile siloxane solvent remains on the skin, a firmly adhering Vaseli ® nfilm in fine Distribution. In Remington's Pharmaceutical Science 15th Edition, Mack Publishing Co., Eaton, Pa. USA, (1975), pp. 1247-48, the usual petrolatum NF as the ointment base are reproduced as petrolatum USP. According to the invention, however, only special VaseliB fractions, the content of white oils of which is less than 20% by weight, are used.
Nach der US-A-4151 272 ist ferner ein Antiperspirantstift bekannt, der aus wachsartigen Fettalkohol, Adstringens, flüchtigem Silicon und bestimmten polyäthoxylierten Fattalkoholen aufgebaut ist. Einerseits muß ein Antiperspirantstift andere Anforderungen erfüllen als eine Salbengrundlage, in der keinerlei Adstringens vorgesehen ist, und darüber hinaus wird in einem derartigen Stift weder Vaseline@ nach die erfindungsgemäß eingesetzte spezielle mit einem Gehalt an Weißölen unter 20 Gew.% angewendet.According to US-A-4151 272 an antiperspirant stick is also known, which is composed of waxy fatty alcohol, astringent, volatile silicone and certain polyethoxylated fatty alcohols. On the one hand, an antiperspirant stick has to meet different requirements than an ointment base in which no astringent is provided, and moreover, in such a stick neither Vaseline @ according to the special invention is used with a content of white oils below 20% by weight.
Die Aufgabe der Erfindung besteht darin, eine auf der Haut gut verteilbare und fest haftende physiologisch unbedenkliche Salbengrundlage zu schaffen, die reizfrei ist und auch bei häufigem Waschen einen lang anhaltenden Schutz bietet.The object of the invention is to provide a physiologically harmless ointment base which is readily distributable and firmly adhering to the skin, which is free from irritation and offers long-lasting protection even with frequent washing.
Es wurde nun gefunden, daß man die bisherigen Nachteile vermeiden kann, wann man bestimmte VaseliRfraktionen mit bestimmten Mengen spezieller, geeigneter, physiologisch unbedenklicher Lösungsmittel vermischt.It has now been found that the previous disadvantages can be avoided when certain Vaseli fractions are mixed with certain amounts of special, suitable, physiologically acceptable solvents.
Gegenstand der Erfindung sind Salbengrundlagen für dermatologische und kosmetische Zwecke auf der Basis von Vaseline@ unter Zusatz von Siloxan, gekennzeichnet durch einen Gehalt an
- a) 10 bis 90 Gew.% Vaselinfraktionen, deren Gehalt an Weißölen unter 20 Gew.% liegt, und
- b) 90 bis 10 Gew.% Octamethylcyclotetrasiloxan, Decamethylcyclopentasiloxan und/oder Hexamethyldisiloxan als Lösungsmittel.
- a) 10 to 90% by weight of petroleum jelly fractions, the white oil content of which is below 20% by weight, and
- b) 90 to 10% by weight of octamethylcyclotetrasiloxane, decamethylcyclopentasiloxane and / or hexamethyldisiloxane as solvent.
Das Vermischen der angegebenen Mengen Lösungsmittel mit der erfolgt zweckmäßig bei leicht erhöhter Temperatur. Beim Abkühlen entsteht ein leicht verstreichbares Präparat.Mixing the specified amounts of solvent with the expediently takes place at a slightly elevated temperature. When cooling, an easily spreadable preparation is created.
Bevorzugt liegt das Verhältnis von Vaseline@ zu Lösungsmittel bei 30 bis 70 Gew.% zu 70 bis 30 Gew.%. Vorzugsweise wird eine verwendet, deren Gewichtsverhältnis von festen zu bei 20 bis 25°C flüssigen Anteilen bei über 3, insbesondere 5 bis 7 liegt. Nach einer besonders bevorzugten Ausführungsform sind in der erfindungsgemäßen Salbengrundlage hochschmelzende Mikrokristallinwachse enthalten.The ratio of Vaseline @ to solvent is preferably 30 to 70% by weight to 70 to 30% by weight. Preferably one used, the weight ratio of solid to liquid at 20 to 25 ° C proportions is over 3, in particular 5 to 7. According to a particularly preferred embodiment, high-melting microcrystalline waxes are contained in the ointment base according to the invention.
Zweckmäßig weist die vorliegende Salbengrundlage als zusätzliche Komponente physiologisch verträgliche niedere Alkohols auf.The present ointment base expediently has physiologically compatible lower alcohol as an additional component.
Die der erfindungsgemäßen Salbengrundlagen besteht aus physiologisch unbedenklichen , deren Gehalt an Weißölen unter 20 Gew.% liegt. Die Weißöle umfassen die niedrigsiedenden, niedrigviskosen, hautreizende Wirkung ausübenden Bestandteile der Vaseline@. Nach Abtrennung der Weißöle, beispielsweise durch Destillation, erhält man somit reizfreie VaseliRfraktionen. Vorzugsweise enthalten die VaseliRfraktionen keine Anteile mit weniger als 20 Kohlenstoffatomen im Molekül. Zur Herstellung der erfindungsgemäß eingesetzten Vaselinfraktionen können beliebige Vaselinen@ verwendet werden. Der Einsatz der vorstehend beschriebenen VaseliRfraktionen, die nur einen geringen Gehalt an Weißölen aufweisen oder aus denen durch Destillation die Weißöle auf den angegebenen Gehalt abgetrennt wurden und somit nur eine geringe Wahrscheinlichkeit einer möglichen Hautreizung besteht, führt in Verbindung mit den gemäß der Erfindung verwendbaren physiologisch unbedenklichen Lösungsmitteln zu stabilen, opaken, dermatologisch günstigen und kosmetisch ansprechenden Zubereitungen.The The ointment bases according to the invention consist of physiologically harmless , whose white oil content is below 20% by weight. The white oils comprise the low-boiling, low-viscosity, skin-irritating components of Vaseline @. After the white oils have been separated off, for example by distillation, irritant-free Vaseli fractions are obtained. The Vaseli fractions preferably contain no portions with less than 20 carbon atoms in the molecule. Any Vaseline @ can be used to produce the Vaseline fractions used according to the invention. The use of the VaseliR fractions described above, which have only a low content of white oils or from which the white oils have been separated to the stated content by distillation and thus have a low probability of possible skin irritation, leads to the use of the physiologically harmless ones which can be used according to the invention Solvents for stable, opaque, dermatologically inexpensive and cosmetically appealing preparations.
Es besonders zweckmäßig, solche Vaseligfraktionen zu verwenden, die ein Gewichtsverhältnis von festen zu bei 20 bis 25°C flüssigen Anteilen von über 3 aufweisen. Insbesonere soll das Verhältnis von festen zu bei 20 bis 25°C flüssigen Anteilen 10:1 nicht übersteigen. Vorzugsweise erhält man derartige durch Extraktion des Rohdestillats mit halogernierten, insbesondere chlorierten Kohlenwasserstoffen.It particularly expedient such Vaseli g fractions to be used which have a weight ratio of solid to 20 to 25 ° C liquid shares above. 3 In particular, the ratio of solid to liquid at 20 to 25 ° C proportions should not exceed 10: 1. Such are preferably obtained by extraction of the crude distillate with halogenated, especially chlorinated hydrocarbons.
Die erfindungsgemäßen Salbengrundlagen enthalten als Lösungsmittel für die angegebenen Hexamethyldisiloxan, Octamethylcyclotetrasiloxan und/oder Decamethylcyclopentasiloxan. Diese Lösungsmittel sind physiologisch verträglich und bilden mit der in der Wärme, d.h. bei oder über dem Schmelzbereich der VaseliRfraktion, klare Lösungen. Vorzugsweise sind die Lösungsmittel beim Abkühlen, z.B. unterhalb von 35°C nur noch beschränkt in den löslich, so daß selbenartige Gemische entstehen. Zudem sind die genannten Lösungsmittel flüchtig und verbleiben nicht auf der Haut. Unter Flüchtigkeit ist zu verstehen, daß die Lösungsmittel aufgrund ihrer geringen Verdampfungswärme innerhalb kurzer Zeit von der Haut abdunsten. Die Lösungsmittel können sowohl einzeln als auch im Gemisch verwendet werden. Die verwendeten Siloxane dienen ausschließlich als Lösungsmittel, um eine gute Verteilung der Vaseline@ auf der Haut zu erreichen, verbleiben aufgrund der Flüchtigkeit jedoch nicht auf der Haut und hinterlassen nach ihrer Verdampfung einen schützenden auf der Haut. Die Flüchtigkeit der angewendeten Lösungsmittel ist neben ihrer Inertheit für die Wirksamkeit der Präparate und den damit erzielbaren Hautschutz von größter Bedutung.The ointment bases according to the invention contain as solvents for the specified Hexamethyldisiloxane, octamethylcyclotetrasiloxane and / or decamethylcyclopentasiloxane. These solvents are physiologically compatible and form with the in the heat, ie at or above the melting range of the Vaseli fraction, clear solutions. When cooling, for example below 35 ° C., the solvents are preferably only limited in the soluble, so that like mixtures are formed. In addition, the solvents mentioned are volatile and do not remain on the skin. Volatility means that the solvents evaporate from the skin within a short time due to their low heat of vaporization. The solvents can be used both individually and in a mixture. The siloxanes used only serve as solvents in order to achieve a good distribution of the Vaseline @ on the skin, but do not remain on the skin due to the volatility and leave a protective layer after they evaporate on the skin. In addition to their inertness, the volatility of the solvents used is extremely important for the effectiveness of the preparations and the skin protection that can be achieved with them.
Nach einer bevorzugten Ausführungsform verwendet man als eine Vaseline@, deren flüssige Anteile gegenüber den festen stark vermindert sind. Dadurch wird ein noch besserer Hautschutz erhalten, da diese Präparate auch unter der Einwirkung von Detergentien einen dauerhaften Hautschutz bilden.According to a preferred embodiment, is used as a Vaseline @, the liquid components of which are greatly reduced compared to the solid ones This will make it even better Preserve skin protection, as these preparations provide permanent skin protection even when exposed to detergents.
Handelsübliche, den Anforderungen der Arzneibücher entsprechende Vaselinen@ bestehen aus ungefähr gleichen Teilen von bei 20 bis 25°C flüssigen und von über 60°C schmelzenden festen Anteilen. Wählt man nun ein Gewichtsverhältnis von festen zu flüssigen Anteilen von über 3, vorzugsweise jedoch 5 bis 7, so erhält man zähe auf der Haut kaum verstreichbare Massen, welche keine den Arzneibüchern entsprechenden Vaselinen@ mehr sind. Durch Zusatz von Octamethylcyclotetrasiloxan, Decamethylcyclopentasiloxan und/oder Hexamethyldisiloxan erhält man jedoch gut verstreichbare, festhaftende Massen. Besonders günstig ist die Kombination von 20 bis 40 Gew.% der angegebenen Siloxane mit 80 bis 60 Gew.% Vaseiinfraktion mit einem Gewichtsverhältnis von festen zu flüssigen Anteilen von 5 bis 7.Commercial vaselines @ corresponding to the requirements of the pharmacopoeias consist of roughly equal parts of solid parts which are liquid at 20 to 25 ° C and melted above 60 ° C. If one now selects a weight ratio of solid to liquid proportions of more than 3, but preferably 5 to 7, then one obtains viscous masses which are hardly vasable on the skin and which are no longer Vaseline @ corresponding to the pharmacopoeias. By adding octamethylcyclotetrasiloxane, decamethylcyclopentasiloxane and / or hexamethyldisiloxane, however, easily spreadable, adherent compositions are obtained. The combination of 20 to 40% by weight of the specified siloxanes with 80 to 60% by weight of vase egg fraction with a weight ratio of solid to liquid proportions of 5 to 7 is particularly favorable.
Ein bei Anwendung dieser Zubereitungen auf der Haut verbleibender Fettglanz kann durch Erhöhung des Anteils der hochschmelzenden Bestandteile der Vaseline@ durch Zufügung von hochschmelzenden Mikrokristallinwachsen praktisch beseitigt werden, ohne die gute Verstreichbarkeit des Präparates zu beeinträchtigen. Hochschmelzende Mikrokristallinwachse mit einem Schmelzbereich von 85 bis 95°C liefern hervorragende Ergebnisse. Durch Zusatz von hochschmelzenden Mikrokristallinwachen (Fp ca. 90°C) im Ausmasse von 5 bis 15 Gew.%, bezogen auf die Summe von Vasefinfraktion und Lösungsmittel, erhält man weiße, opake Massen, die auf der Haut verstrichen gut haften und kaum noch Glanz hinterlassen. Dies ist überraschend, werden doch Mikrokristallinwachse sonst zur Glanzerhöhung, insbesondere bei Parafinwachsen, eingesetzt.A greasy gloss remaining on the skin when these preparations are used can be practically eliminated by increasing the proportion of high-melting constituents of the Vaseline @ by adding high-melting microcrystalline waxes without impairing the good spreadability of the preparation. High-melting microcrystalline waxes with a melting range of 85 to 95 ° C deliver excellent results. By adding high-melting microcrystalline guards (melting point approx. 90 ° C) in the amount of 5 to 15% by weight, based on the sum of vasefine fraction and solvent, white, opaque masses are obtained which adhere well to the skin and hardly any shine leave. This is surprising, since microcrystalline waxes are otherwise used to increase the gloss, particularly in the case of paraffin waxes.
Gegebenenfalls können die erfindungsgemäßen Zubereitungen noch weitere physiologisch verträgliche Zusätze enthalten. Dabei sind Zusätze in geringen Mengen, z.B. bis zu 5%, geeignet. Bevorzugt wird die Zugabe von physiologisch unbedenklichen niedrigen Alkoholen, wie z.B. Äthyl- und lsopropylalkohol. Werden bei der Herstellung geringe Mengen derartiger Zusätze zugegeben, so erhält man besonders leicht verstreichbare, kosmetisch ansprechende Zubereitungen, die matt und nicht glänzend auftrocknen und zudem einen oftmals erwünschten Abkühlungseffekt aufweisen. Ferner können weitere übliche Zusätze in den erfindungsgemäßen Zubereitungen enthalten sein, soweit sie physiologisch unbedecklich sind und mit den verwendeten Lösungsmitteln verträglich sind. Beispiele derartiger Zusätze sind UV-Adsorber, Geruchstoffe und Verdickungsmittel wie z.B. Ceresin, Ozokerit, Aluminiumstearat, Polyvinlylstearat und Polyvinylpyrrolidonderivate, sodann, zur Modifikation des Hautgefühls, Isopropylester von Fettsäuren wie Isopropylmyristat und Lanolinderivate.If appropriate, the preparations according to the invention can also contain further physiologically tolerable additives. Additions in small amounts, e.g. up to 5%, suitable. It is preferred to add physiologically acceptable lower alcohols, e.g. Ethyl and isopropyl alcohol. If small amounts of such additives are added in the production, then particularly easily spreadable, cosmetically appealing preparations are obtained which dry matt and not glossy and also have a cooling effect which is often desired. Furthermore, other customary additives can be contained in the preparations according to the invention, provided that they are physiologically unsuitable and are compatible with the solvents used. Examples of such additives are UV adsorbers, odorants and thickeners such as e.g. Ceresin, ozokerite, aluminum stearate, polyvinyl stearate and polyvinyl pyrrolidone derivatives, then, to modify the feeling on the skin, isopropyl esters of fatty acids such as isopropyl myristate and lanolin derivatives.
Die Menge der inagesamt in der erfindungsgemäßen Salbengrundlage vorliegenden Zusätze soll vorzugsweise 20 Gew.%, bezogen auf die Summe von Vasetinfraktion und Siloxanlösungsmittel, nicht überschreiten.The total amount of additives present in the ointment base according to the invention should preferably not exceed 20% by weight, based on the sum of the vasetin fraction and the siloxane solvent.
Die aus den und den angegebenen Siloxanlösungsmitteln in den aufgeführten Mengenverhältnissen sowie gegegenenfalls weiteren Zusätzen aufgebauten Zubereitungen sind hervorragende Salbengrundlagen und ausgezeichnete Hautpflege- und Hautschutzpräparate, die sich auf der Haut leicht verstreichen lassen und auch in den tieferen Teil der Hornhaut, welcher bei den weißrassigen Menschen aus etwa 16 Zellschichten besteht, eindringen. Dies ist begreiflich, weil die Abmessungen der gelösten Vaselillmoleküle einige Zehnerpotenzen unter der Größe der dispersen Phase von Emulsionen liegen. Nach Abdunsten des Lösungsmittels bleibt ein Kohlenwasserstoffgemisch zurück, das sich auch durch mehrmaliges Waschen der Haut mit Seife oder Syndets nicht mehr vollständig entfernen läßt. Solchermaßen geschützte Haut setzt dem Durchgang von Wasser in beiden Richtungen und somit auch dem Eindrigen von wasserlöslichen Noxen großen Widerstand entgegen. Da das unverseifbar ist und chemische Noxen meist in wäßriger Lösung, oft bei höheren pH-Werten und/oder in Gegenwart von Netzmitteln vorliegen (z.B. Hauschaltswaschmittel oder thioglykolsäurehaltige Kaltwellpräparate), entfalten die erfindungsgemäßen Zubereitungen eine ausgezeichnete Schutzwirkung für die Haut.The from the and the specified siloxane solvents in the proportions listed and, if necessary, other additives built up preparations are excellent ointment bases and excellent skin care and skin protection products that can be easily spread on the skin and also in the deeper part of the cornea, which in the white-blooded people from about 16 cell layers exists, penetrate. This is understandable because the dimensions of the dissolved Vaselill molecules are a few orders of magnitude smaller than the size of the disperse phase of emulsions. After the solvent has evaporated, a hydrocarbon mixture remains, which cannot be completely removed even by washing the skin several times with soap or syndets. Skin protected in this way offers great resistance to the passage of water in both directions and thus also to the penetration of water-soluble noxae. Since that is unsaponifiable and chemical noxae are usually present in aqueous solution, often at higher pH values and / or in the presence of wetting agents (e.g. household detergents or thioglycolic acid-containing cold wave preparations), the preparations according to the invention have an excellent protective action for the skin.
Da die erfindungsgemäßen wasserfreien Präparate keinerlei Konservierungsmittel benötigen, lassen sich auch durch solche Wirkstoffe bedingte Allergien vermeiden. Durch den Einsatz von Hexamethyldisiloxan, Octamethylcyclotetrasiloxan und/oder Decamethylcyclopentasiloxan als Lösungsmittel, die olfaktorisch kaum wahrnehmbar sind, lassen sich bei entsprechender Wahl der praktisch geruchlose Präparate erhalten, die keinerlei Geruchskorrigentien bedürfen. Dadurch lassen sich allergische und phototoxische Erscheinungen wie sie bei der Anwendung von Riechstoffen auftreten können, vermeiden. Dies ist besonders wichtig, wenn erfindungsgemäß hergestellte Zubereitungen unter Zufügung von geeigneten UV-Absorbern als Sonnenschutzmittel dienen sollen. Dazu eignen sie sich hervorragend, weil die Vaseline@ an sich schon Sonnenschutzeignachaften hat und weil das emulgatorfreie Präparat beim Baden nicht ausgewaschen und vom Sand mechanisch kaum abgetragen wird. Man erhält damit lange wirksame Sonnenschutzpräparate, was vom Standpunkt des Lichtschutzes der Haut von großer Wichtigkeit ist.Since the water-free preparations according to the invention do not require any preservatives, allergies caused by such active ingredients can also be avoided. Through the use of hexamethyldisiloxane, octamethylcyclotetrasiloxane and / or decamethylcyclopentasiloxane as solvents, which are hardly noticeable olfactively, the choice can be made with the appropriate choice receive practically odorless preparations that do not require any odor corrections. This avoids allergic and phototoxic phenomena that can occur when using fragrances. This is particularly important if preparations made according to the invention are to serve as sunscreens with the addition of suitable UV absorbers. They are ideal for this because the petroleum jelly has inherent sun protection properties and because the emulsifier-free preparation is not washed out during bathing and is hardly mechanically removed from the sand. This provides long-lasting sunscreen preparations, which is very important from the point of view of protecting the skin from light.
Sodann ist die Geruchsfreiheit von Handschutzpräparaten ein Erfordernis, wenn die Hände danach mit Lebensmitteln in Berührung kommen, weil die Möglichkeit einer unerwünschten Geruchsübertragung bei parfümierten Produkten besteht. Die erfindungsgemäßen Präparate eignen sich auch in besonderer Weise als Gewerbeschutzcreme.
Die beiden Komponenten werden erwämt bis eine klare Lösung entstanden ist, hernach wird kaltgerührt.
Die Komponenten werden erwärmt bis eine klare Lösung entstanden ist, anschließend wird kaltgerührt.
Die Komponenten werden erwärmt bis eine klare Lösung entstanden ist, anschließend wird kaltgerührt.The components are heated until a clear solution is obtained, then the mixture is stirred until cold.
Sämtliche in den vorstehenden Beispielen hergestellte Präparate ergeben hervorragenden Hautschutz.
Die ersten 3 Anteile werden in einem mit einem Rückflußkühler versehenen, heizbaren Gefäß bei ca. 95°C geschmolzen, und nachdem eine homogene Lösung entstanden ist, wird das Octamethylcyclotetrasiloxan beigefügt und unter schwachem Rühren abgekühlt. Nach Stehenlassen während 24 Std. bildet sich ein reinweißes Lipogel, das sich auf der Haut leicht verstreichen läßt und die damit behandelten Hände sehr stark hydrophobisiert. Die anzuwendende Menge ist gering: 0,3 bis 0,5 g sind für einen Hautschutz während eines ganzes Arbeitstages im allgemeinen ausreichend.
Die Harstellung erfolgt in gleicher Weise wie bei Beispiel 4. Die entstandene Zubereitung ergibt auf der Hand verstrichen ein besondere angenehmes Hautgefühl.
Die Herstellung erfolgt in gleicher Weise wie bei Beispiel 4. Die erhaltene Zubereitung läßt sich auf der Haut leicht zu einem dünnen, matt auftrocknenden Film verstreichen, der auch bei häufigem Waschen auf der Haut als Schutz verbleibt.
Die Komponenten werden erwärmt, bis eine klare Lösung entstanden ist, anschließend wird kaltgerührt.The components are heated until a clear solution is obtained, then the mixture is stirred until cold.
Das erhaltene Präparat ist auf der Haut gut verstreichbar und liefert einen lang anhaltenden Hautschutz.The preparation obtained is easy to spread on the skin and provides long-lasting skin protection.
Claims (5)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| AT81102009T ATE14675T1 (en) | 1980-03-19 | 1981-03-18 | OINTMENT BASES FOR DERMATOLOGICAL AND COSMETIC PURPOSES. |
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE3010572A DE3010572C2 (en) | 1980-03-19 | 1980-03-19 | Skin care and skin protection preparations |
| DE3010572 | 1980-03-19 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| EP0037011A2 EP0037011A2 (en) | 1981-10-07 |
| EP0037011A3 EP0037011A3 (en) | 1982-07-21 |
| EP0037011B1 true EP0037011B1 (en) | 1985-08-07 |
Family
ID=6097687
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EP81102009A Expired EP0037011B1 (en) | 1980-03-19 | 1981-03-18 | Ointment bases for dermatological and cosmetic use |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US4355046A (en) |
| EP (1) | EP0037011B1 (en) |
| JP (1) | JPS56145212A (en) |
| AT (1) | ATE14675T1 (en) |
| DE (2) | DE3010572C2 (en) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS59225111A (en) * | 1983-06-07 | 1984-12-18 | Kao Corp | Composition for cleaning and wiping skin around anus |
| US4578266A (en) * | 1983-07-29 | 1986-03-25 | Revlon, Inc. | Silicone-based cosmetic products containing pigment |
| CA1244351A (en) * | 1983-07-29 | 1988-11-08 | Radhakrishna B. Kasat | Antiperspirant creams |
| US4574082A (en) * | 1983-07-29 | 1986-03-04 | Revlon, Inc. | One-phase silicone-based cosmetic products containing wax |
| US4678663A (en) * | 1984-02-06 | 1987-07-07 | Nuetrogena Corporation | Hydroquinone composition having enhanced bio-availability and percutaneous adsorption |
| FI872553L (en) * | 1986-06-09 | 1987-12-10 | American Cyanamid Co | MEDIUM FOER LAEKEMEDEL FOER LOKALT BRUK. |
| FI872552L (en) * | 1986-06-09 | 1987-12-10 | American Cyanamid Co | PROSTAGLANDINKOMPOSITION FOER LOKALT BRUK. |
| DE3640177A1 (en) * | 1986-11-25 | 1988-05-26 | Bayer Ag | SKIN PROTECTIVE OR SKIN CARE COMPOSITION |
| US4960764A (en) * | 1987-03-06 | 1990-10-02 | Richardson-Vicks Inc. | Oil-in-water-in-silicone emulsion compositions |
| PH25566A (en) * | 1987-04-01 | 1991-08-08 | Plough | Non-aqueous suncare composition having high spf values |
| DE3918615C2 (en) * | 1989-06-07 | 1995-07-27 | Woellner Werke | Skin protection cream based on an aqueous emulsion |
| US4988503A (en) * | 1990-01-24 | 1991-01-29 | Revlon, Inc. | Oil-in-water emulsions for foundation makeup composition |
| US5145875A (en) * | 1990-03-05 | 1992-09-08 | Dow Corning Corporation | Glyceroxyfunctional silanes and siloxanes |
| US5043359A (en) * | 1990-03-05 | 1991-08-27 | Dow Corning Corporation | Skin conditioning compositions containing glyceroxyfunctional silanes and siloxanes |
| DE4117887C2 (en) * | 1990-06-09 | 1993-12-16 | Siegfried Rochler | Use of pharmaceutically / cosmetically defined petroleum jelly as a nasal ointment for the prophylaxis of inhalation allergic reactions |
| US5336692A (en) * | 1990-06-28 | 1994-08-09 | Medicis Pharmaceutical Corporation | Ointment base and method of use |
| US5085855A (en) * | 1990-07-18 | 1992-02-04 | Mary Kay Cosmetics, Inc. | Silicone based cosmetic product |
| US6515029B1 (en) | 1999-04-23 | 2003-02-04 | Kimberly-Clark Worldwide, Inc. | Absorbent article having a hydrophilic lotionized bodyside liner |
| US6375942B1 (en) | 1999-08-31 | 2002-04-23 | Michael C. Rico | Skin healing ointment |
| DE20009841U1 (en) * | 2000-05-31 | 2001-10-25 | Phyt-Immun GmbH, 66424 Homburg | Vaseline-based nasal ointment |
| US6503526B1 (en) | 2000-10-20 | 2003-01-07 | Kimberly-Clark Worldwide, Inc. | Absorbent articles enhancing skin barrier function |
| US6756520B1 (en) | 2000-10-20 | 2004-06-29 | Kimberly-Clark Worldwide, Inc. | Hydrophilic compositions for use on absorbent articles to enhance skin barrier |
| US7771735B2 (en) | 2000-12-22 | 2010-08-10 | Kimberly-Clark Worldwide, Inc. | Absorbent articles with compositions for reducing irritation response |
| US20020128615A1 (en) | 2000-12-22 | 2002-09-12 | Tyrrell David John | Absorbent articles with non-aqueous compositions containing anionic polymers |
| US6749860B2 (en) | 2000-12-22 | 2004-06-15 | Kimberly-Clark Worldwide, Inc. | Absorbent articles with non-aqueous compositions containing botanicals |
| DE10156297A1 (en) * | 2001-11-19 | 2003-05-28 | Henkel Kgaa | Skin protectant, especially hand cream, which remains in place for long periods comprising paraffin oils, petrolatum, carnauba wax and optionally silicon oils and/or additional waxes |
| US20070258935A1 (en) * | 2006-05-08 | 2007-11-08 | Mcentire Edward Enns | Water dispersible films for delivery of active agents to the epidermis |
| US20070259029A1 (en) * | 2006-05-08 | 2007-11-08 | Mcentire Edward Enns | Water-dispersible patch containing an active agent for dermal delivery |
| US20080057090A1 (en) * | 2006-09-01 | 2008-03-06 | Mcentire Edward Enns | Wrinkle masking film composition for skin |
| US7879942B2 (en) | 2006-10-05 | 2011-02-01 | Eastman Chemical Company | Switchable adhesive article for attachment to skin and method of using the same |
| HUP0900072A2 (en) | 2009-02-06 | 2010-09-28 | Egis Gyogyszergyar Nyilvanosan | Transdermal pharmaceutical compositions |
| US8865194B1 (en) * | 2007-12-20 | 2014-10-21 | Theraplex Company, LLC | Reducing tackiness and greasiness of petrolatum-like materials |
| US9283173B2 (en) * | 2008-01-08 | 2016-03-15 | M.D. Lederman Consulting Ltd. | Emulsified wax compositions and uses thereof |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2727846A (en) * | 1951-08-22 | 1955-12-20 | Silicote Corp | Siloxane-containing dressing |
| GB714795A (en) * | 1952-04-10 | 1954-09-01 | Silicote Corp | Medical dressing |
| DE1134478B (en) * | 1959-05-07 | 1962-08-09 | Schenley Ind Inc | Skin protection ointment containing silicone |
| US3953591A (en) * | 1974-04-29 | 1976-04-27 | The Procter & Gamble Company | Fatty acid, polysiloxane and water-soluble polymer containing skin conditioning emulsion |
| CA1089368A (en) * | 1976-08-02 | 1980-11-11 | Daniel C. Geary | Polyethoxylated fatty alcohol in antiperspirant sticks |
| US4280994A (en) * | 1977-02-10 | 1981-07-28 | Union Carbide Corporation | Antiperspirant stick compositions |
| US4278655A (en) * | 1979-03-07 | 1981-07-14 | Finetex, Inc. | Antiperspirant composition |
-
1980
- 1980-03-19 DE DE3010572A patent/DE3010572C2/en not_active Expired
-
1981
- 1981-03-09 US US06/241,512 patent/US4355046A/en not_active Expired - Lifetime
- 1981-03-17 JP JP3861581A patent/JPS56145212A/en active Pending
- 1981-03-18 EP EP81102009A patent/EP0037011B1/en not_active Expired
- 1981-03-18 AT AT81102009T patent/ATE14675T1/en active
- 1981-03-18 DE DE8181102009T patent/DE3171653D1/en not_active Expired
Non-Patent Citations (2)
| Title |
|---|
| Remington's Pharmaceutical Sciences,15th Ed, Mack Pub. (1975) S. 1247-48 * |
| Römpps Chemie-Lexikon, Neumüller, Franckh'sche Verlag(1977),S.3780 * |
Also Published As
| Publication number | Publication date |
|---|---|
| US4355046A (en) | 1982-10-19 |
| DE3010572A1 (en) | 1981-09-24 |
| JPS56145212A (en) | 1981-11-11 |
| DE3010572C2 (en) | 1982-05-06 |
| EP0037011A2 (en) | 1981-10-07 |
| ATE14675T1 (en) | 1985-08-15 |
| DE3171653D1 (en) | 1985-09-12 |
| EP0037011A3 (en) | 1982-07-21 |
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